Syntheses and Cytotoxicity of Pt(II) Complexes with Acyclovir
Sabina Grabnera*, Maja Čemažarb, Nataša Bukoveca, Gregor Seršab
aFaculty of
Chemistry and Chemical Technology, University of Ljubljana, Aškerčeva 5, 1000
Ljubljana, Slovenia
bDepartment of Experimental Oncology, Institute of Oncology
Ljubljana, Zaloška 2, 1000 Ljubljana, Slovenia
E-mail:
sabina.grabner@fkkt.uni-lj.si
Absrtract
Acyclovir is an antiviral drug which acts against the viruses,
including Herpes simplex 1 and 2 and Varicella-zoster. The novel cis-[PtI2(3-Hmpy)2](3-Hmpy=3-hydroxymethylpyridine)(2)
and the water-soluble cationic Pt(II) complexes with acyclovir (acv, (9-[(2-hydroxyetoxy)methyl]guanine)),
cis-[Pt(acv-N7)2(NH3)2]Cl2·2H2O
(1) and cis-[Pt(acv-N7)2(3-Hmpy)2](NO3)2
(3), have been prepared and characterized by multinuclear NMR spectroscopy. The
results of cytotoxicity assay of 1, 3 and cis-[PtCl2(NH3)2]
(cisplatin, cDDP) performed in malignant melanoma B16 cells in vitro provide
evidence that complex 1 and 3 are less cytotoxic compared to cisplatin. In vivo
experiments performed on the same malignant melanoma B16 cells, grown as
subcutaneous tumours, demonstrated that antitumour effectiveness of 1 was
comparable to that of cisplatin.